抗HIV药物的最新研究进展
发布时间：2018-08-28 11:08
【摘要】：目前多种抗逆转录病毒准新药正在2、3期临床评价中。新的核苷逆转录酶抑制剂tenofoviralafenamidefumarate(TAF)比替诺福韦(tenofovir,TDF)抗病毒活性强且毒性较低;非核苷逆转录酶抑制剂doravirine对该酶耐受病毒株有效,而新的整合酶抑制剂GSK744具有长效的特点。此外,几个具有新的作用机制的化合物也受到关注,如BMS-663 068小分子化合物是CD4结合的抑制剂,而cenicriviroc是新颖的CCR5/CCR2受体拮抗剂,具有抗HIV和抗炎的双重作用。几类针对潜伏病毒感染的药物也正在研发中,其中组蛋白去乙酰化酶抑制剂发展较快,其余大多处于体外筛选阶段,如蛋白激酶C激活剂、DNA甲基转移酶抑制剂、阳性转录延长因子激活剂和组蛋白甲基转移酶抑制剂等。本文对有望近期进入临床使用的新药和可能逆转HIV潜伏感染的化合物进行重点介绍。
[Abstract]:At present, a variety of anti-retroviral quasi-new drugs are in phase 2 3 clinical evaluation. The new nucleoside reverse transcriptase inhibitor (tenofoviralafenamidefumarate (TAF) has stronger antiviral activity and lower toxicity than that of tenofovir (tenofovir,TDF), and the non-nucleoside reverse transcriptase inhibitor (doravirine) is effective against the strain, while the new integrase inhibitor GSK744 has a long effect. In addition, several compounds with new mechanism of action are also concerned, such as BMS-663 068 small molecule compound is an inhibitor of CD4 binding, while cenicriviroc is a novel CCR5/CCR2 receptor antagonist with both anti-HIV and anti-inflammatory effects. Several kinds of drugs for latent virus infection are also under development, among which histone deacetylase inhibitors develop rapidly, and the rest are mostly in the screening stage in vitro, such as protein kinase C activator, DNA methyltransferase inhibitor, Positive activator of transcription extension factor and histone methyltransferase inhibitor. This article focuses on new drugs and compounds that could reverse latent infection of HIV in the near future.
【作者单位】： 加州大学圣地亚哥医学院传染病系;
【分类号】：R978.7
，
本文编号：2209215
[Abstract]:At present, a variety of anti-retroviral quasi-new drugs are in phase 2 3 clinical evaluation. The new nucleoside reverse transcriptase inhibitor (tenofoviralafenamidefumarate (TAF) has stronger antiviral activity and lower toxicity than that of tenofovir (tenofovir,TDF), and the non-nucleoside reverse transcriptase inhibitor (doravirine) is effective against the strain, while the new integrase inhibitor GSK744 has a long effect. In addition, several compounds with new mechanism of action are also concerned, such as BMS-663 068 small molecule compound is an inhibitor of CD4 binding, while cenicriviroc is a novel CCR5/CCR2 receptor antagonist with both anti-HIV and anti-inflammatory effects. Several kinds of drugs for latent virus infection are also under development, among which histone deacetylase inhibitors develop rapidly, and the rest are mostly in the screening stage in vitro, such as protein kinase C activator, DNA methyltransferase inhibitor, Positive activator of transcription extension factor and histone methyltransferase inhibitor. This article focuses on new drugs and compounds that could reverse latent infection of HIV in the near future.
【作者单位】： 加州大学圣地亚哥医学院传染病系;
【分类号】：R978.7
，
本文编号：2209215
本文链接：https://www.wllwen.com/yixuelunwen/yiyaoxuelunwen/2209215.html
最近更新
教材专著
